Table 1

Thermodynamic parameters of VEGF/VEGFR-2 interactions determined by ITC*

NKd, μMΔG, kcal/molΔH, kcal/mol−TΔS, kcal/molc
VEGF-A121/VEGFR-2 D23 2.01 0.093 −8.9 6.6 −15.5 281 
VEGF-A165/VEGFR-2 D23 1.89 0.17 −8.6 6.5 −15.1 150 
VEGF-C/VEGFR-2 D23 1.91 0.20 −8.5 12.0 −20.5 131 
VEGF-E/VEGFR-2 D23 2.21 0.28 −8.3 13.2 −21.5 91 
VEGF-A121/VEGFR-2 ECD 1.97 1.12 −7.5 10.4 −17.9 57 
VEGF-A165/VEGFR-2 ECD 2.06 2.67 −7.1 12.5 −19.6 24 
VEGF-C/VEGFR-2 ECD 1.9 1.21 −7.5 14.8 −22.3 53 
VEGF-E/VEGFR-2 ECD 2.09 5.99 −6.6 17.7 −24.3 11 
   ΔΔG, kcal/mol ΔΔH, kcal/mol −TΔΔS, kcal/mol 
VEGF-A121 1.4 3.8 −2.4 
VEGF-A165 1.5 6.0 −4.5 
VEGF-C 1.0 2.8 −1.8 
VEGF-E 1.7 4.5 −2.8 
NKd, μMΔG, kcal/molΔH, kcal/mol−TΔS, kcal/molc
VEGF-A121/VEGFR-2 D23 2.01 0.093 −8.9 6.6 −15.5 281 
VEGF-A165/VEGFR-2 D23 1.89 0.17 −8.6 6.5 −15.1 150 
VEGF-C/VEGFR-2 D23 1.91 0.20 −8.5 12.0 −20.5 131 
VEGF-E/VEGFR-2 D23 2.21 0.28 −8.3 13.2 −21.5 91 
VEGF-A121/VEGFR-2 ECD 1.97 1.12 −7.5 10.4 −17.9 57 
VEGF-A165/VEGFR-2 ECD 2.06 2.67 −7.1 12.5 −19.6 24 
VEGF-C/VEGFR-2 ECD 1.9 1.21 −7.5 14.8 −22.3 53 
VEGF-E/VEGFR-2 ECD 2.09 5.99 −6.6 17.7 −24.3 11 
   ΔΔG, kcal/mol ΔΔH, kcal/mol −TΔΔS, kcal/mol 
VEGF-A121 1.4 3.8 −2.4 
VEGF-A165 1.5 6.0 −4.5 
VEGF-C 1.0 2.8 −1.8 
VEGF-E 1.7 4.5 −2.8 

N indicates the stoichiometry of ligand/receptor complexes.

*

Error estimation: N, ± 0.01; Kd, ± 5%; ΔG, ΔH, and −TΔS, ± 0.5 kcal mol−1.

The c value is calculated as: c = N*[R2]/Kd.

ΔΔ values represent the difference between the ΔG/ΔH/−TΔS values between the full-length ECD and the D23 ligand complexes.

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